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Small Molecule MRS5474 with Anticonvulsant Activity for Treatment of Epilepsy

Posted Nov 15 2012 7:00pm

Description of Invention:
Adenosine modulates many physiological processes by activating specific adenosine receptors. These adenosine receptors play a critical role in the regulation of cellular signaling and are broadly distributed throughout the body. Thus, the ability to modulate adenosine receptor-mediated signaling is an attractive therapeutic strategy for a broad range of diseases. This technology relates to a group of compounds that display high affinity and specificity for the A1 adenosine receptor subtype.

One of the compounds, MRS5474, displays anticonvulsant activity in the 6 Hz animal model of clonic seizures. In the minimal behavioral toxicity test using the rotarod, no toxicity (zero out of eight mice) was observed at all doses tested up to 30 mg/kg, the highest dose tested, which was nearly completely protective (seven out of eight animals) in the 6 Hz model. MRS 5474 also tested well in the corneal kindled mouse model to examine its effect on focal seizures.

  • Oral anticonvulsant drug.
  • Provides a means to mimic A1AR mediated signaling in vitro and in vivo.

  • These small molecules display increased specificity for the A1 type of adenosine receptors, which may reduce unwanted side effects previously seen in A1AR agonist therapies.
  • The physical properties of these molecules are drug-like, which makes them attractive for pre-clinical development.

Development Status:
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)

Kenneth A Jacobson (NIDDK)
Dilip K Tosh (NIDDK)

Patent Status:
HHS, Reference No. E-285-2008/1
US, Application No. 13/479,973 filed 24 May 2012

Related Technologies:
US, Application No. 61/085,588 filed 01 Aug 2008, Reference No. E-285-2008/0
US, Application No. 13/056,997 filed 31 Jul 2009, Reference No. E-285-2008/0

Relevant Publication:
  1. Tosh DK, et al. Truncated (N)-Methanocarba Nucleosides as A1 Adenosine Receptor Agonists and Partial Agonists: Receptor Docking and Potent Anticonvulsant Activity. In preparation.

Collaborative Research Opportunity:
The NIDDK is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize MRS5474, A1 adenosine receptor agonist for treatment of seizures. For collaboration opportunities, please contact Marguerite Miller at .

For Licensing Information Please Contact:
Betty Tong Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-594-6565
Fax: 301-402-0220

Ref No: 2500

Updated: 11/2012

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